The isolation of pancratistatin was disclosed in U.S. Letters Pat. No. 4,985,436 issued Jan. 15, 1991. The general background therefrom relating to pancratistatin is incorporated herein, by this reference hereto, as if fully set forth.
As was noted in the above patent, pancratistatin is at best sparingly soluble in water. This substantially limits the availability of this drug in a form that could be administered in an aqueous solution. This has become significant since pancratistatin has been selected by the National Cancer Institute for pre-clinical development. Accordingly, the synthesis of a pancratistatin prodrug is important.
Therefore, the prime objective of the subject invention is to disclose the discovery of a disodium phosphate prodrug salt of pancratistatin which is a bioequivalent thereof.